Table 1 In vitro ADME properties of EGT710

From: Preclinical characterization of EGT710, an oral non-peptidomimetic reversible covalent SARS-CoV-2 main protease inhibitor

Property

Value

Papp MDCK-LE (x10-6 cm s−1)

21.4

MDCK-MDR1 (x10-6 cm s-1) PappA-B / PappB-A / ER

7.4 / 13.0 / 1.8

Clint, microsomes (µL/min/mg) (M/Rt/D/H)

<10 / < 10 / 13.3 / < 10

Clint, hepatocytes (µL/min/million cells) (M/Rt/D/H)

5.2 / < 4 / < 4 / < 4

Plasma protein binding (%) (M/Rt/Rb/D/H)a

81.9 / 86.1 / 74.3 / 76.1 / 88.2

Binding to dNHBE media (%)

2.82

Cb/Cp (M/Rt/Rb/D/H)b

0.83 / 1.10 / 1.49 / 0.92 / 1.21

  1. Papp apparent permeability coefficient, MDCK-LE Madin-Darby canine kidney low efflux cells, MDCK-MDR1 Madin-Darby canine kidney cells expressing multidrug resistance 1, CLint intrinsic clearance, M/Rt/Rb/D/H mouse/rat/rabbit/dog/human, Cb/Cp blood to plasma ratio.
  2. aPPB values from discovery-stage rat assay are reported in ref. 7 here, we report PPB values from IND-enabling assays for all species. Mean values for experiments performed at 1 and 10 µM are reported.
  3. bMean values for experiments performed at 10, 100, 1000, and 10,000 ng/mL are reported.
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